Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs

…, X Chen, P Zhan, E De Clercq, C Pannecouque…

Index: Rai, Diwakar; Chen, Wenmin; Tian, Ye; Chen, Xuwang; Zhan, Peng; De Clercq, Erik; Pannecouque, Christophe; Balzarini, Jan; Liu, Xinyong Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 23 p. 7398 - 7405

Full Text: HTML

Citation Number: 2

Abstract

Abstract A novel series of 3-benzyloxy-linked pyrimidinylphenylamine derivatives (8a–8s) was designed, synthesized and evaluated for their in vitro anti-HIV activity in MT-4 cell cultures. Most of the compounds inhibited wild-type (wt) HIV-1 replication in the lower micromolar concentration range (EC 50= 0.05–35 μM) with high selectivity index (SI) values (ranged from 10 to> 4870). In particular, 8h and 8g displayed excellent antiretroviral ...

Related Articles:

Metallo-β-lactamase-Catalyzed Hydrolysis of Cephalosporins: Some Mechanistic Insights into the Effect of Heterocyclic Thiones on Enzyme Activity

[Katritzky, Alan R.; Baykut, Gokhan; Rachwal, Stanislaw; Szafran, Miroslaw; Caster, Kenneth C.; Eyler, John Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999), 1989 , p. 1499 - 1506]

Fluorinated heterocyclic compounds. 2. 2, 4??difluoro and 4??amino??2??fluoropyrimidines, nucleoside base analogs

[Journal of Heterocyclic Chemistry, , vol. 22, p. 149 - 153]

Structural tuning of ancillary chelate in tri-carboxyterpyridine Ru (II) sensitizers for dye sensitized solar cells

[Journal of Materials Chemistry A, , vol. 2, # 15 p. 5418 - 5426]

More Articles...